H2 receptor antagonists

Ranitidine, sold under the brand name Zantac among others, is a medication used to decrease stomach acid production. It is used in the treatment of peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. It can be given by mouth, injection into a muscle, or injection into a vein.

Olanzapine, sold under the brand name Zyprexa among others, is an atypical antipsychotic primarily used to treat schizophrenia and bipolar disorder. It is also sometimes used off-label in cancer patients for treatment of chemotherapy-induced nausea and vomiting and as an appetite stimulant. For schizophrenia, it can be used for both new-onset disease and long-term maintenance. It is taken by mouth or by injection into a muscle.

Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid production. It is mainly used in the treatment of heartburn and peptic ulcers.

Famotidine, sold under the brand name Pepcid among others, is a histamine H2 receptor antagonist medication that decreases stomach acid production. It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. It is taken by mouth or by injection into a vein. It begins working within an hour.

drugs that selectively bind to but do not activate histamine H2 receptors

Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine which is used to treat allergies. In addition, it has a number of off-label uses, such as treatment of serotonin syndrome, insomnia, and use as an appetite stimulant. The drug is taken orally.

Nizatidine is a histamine H2 receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease.

Lafutidine (INN) is a second generation histamine H2 receptor antagonist having multimodal mechanism of action and used to treat gastrointestinal disorders. It is marketed in South Korea, Japan and India.

Burimamide is an antagonist at the H2 and H3 histamine receptors. At physiological pH, it is largely inactive as an H2 antagonist, but its H3 affinity is 100x higher. It is a thiourea derivative.

Ebrotidine is an H2 receptor antagonist with gastroprotective activity against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine, and approximately 10-fold greater than those of cimetidine. Ebrotidine has anti-Helicobacter pylori activity via inhibition of the urease enzyme and the proteolytic and mucolytic activities of the bacterium. However, its activity is synergistic with a number of antibacterial agents. Ebrotidine counteracts the inhibitory effects of H. pylori lipopolysaccharides. Ebrotidine was wi

Metiamide is a histamine H2 receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine (Tagamet).

Lavoltidine (INN, USAN, BAN; previously known as loxtidine; development code AH-23,844) is a highly potent and selective H2 receptor antagonist which was under development by Glaxo Wellcome (now GlaxoSmithKline) as a treatment for gastroesophageal reflux disease but was discontinued due to the discovery that it produced gastric carcinoid tumors in rodents.

Niperotidine is a histamine antagonist selective for the H2 subtype. It was studied as a treatment for excessive gastric acidity, but withdrawn after human trials showed liver damage.

Lupitidine (INN; lupitidine hydrochloride (USAN); development code SKF-93479) is a long-acting H2 receptor antagonist developed by Smith, Kline & French and described as an antiulcerogenic that was never marketed. It was shown to inhibit nocturnal gastric acid secretion and, in experiments on rodents, produced diffuse neuroendocrine cell hyperplasia and an increase in multifocal glandular hyperplasia due to hypergastrinemia resulting from the pharmacological suppression of gastric acid secretion.

chemical compound

Zolantidine is a brain-penetrating selective histamine H2 receptor (HRH2) antagonist developed by Smith, Kline & French, with the research code of SK&F 95282. It is a benzothiazole derivative with a 30-fold higher potency for H2 receptors than other peripheral and central receptors.

Fanetizole is a drug that has immunoregulating activity.

Oxmetidine (development code SKF 92994) is an H2 histamine receptor receptor antagonist.